PE20171095A1 - NOVEL FATTY ACIDS AND THEIR USE IN CONJUGATION WITH BIOMOLECULES - Google Patents

NOVEL FATTY ACIDS AND THEIR USE IN CONJUGATION WITH BIOMOLECULES

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Publication number
PE20171095A1
PE20171095A1 PE2016002771A PE2016002771A PE20171095A1 PE 20171095 A1 PE20171095 A1 PE 20171095A1 PE 2016002771 A PE2016002771 A PE 2016002771A PE 2016002771 A PE2016002771 A PE 2016002771A PE 20171095 A1 PE20171095 A1 PE 20171095A1
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Peru
Prior art keywords
biomolecules
conjugation
fatty acids
acid
novel fatty
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Application number
PE2016002771A
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Spanish (es)
Inventor
Chikwendu Ibebunjo
Alexandra Marshall Bruce
Avirup Bose
David Weninger Barnes
Ken Yamada
Aaron Kanter
Alokesh Duttaroy
Louise Clare Kirman
Aimee Richardson Usera
Frederic Zecri
Jun Yuan
Changgang Lou
Original Assignee
Novartis Ag
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Application filed by Novartis Ag filed Critical Novartis Ag
Publication of PE20171095A1 publication Critical patent/PE20171095A1/en

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    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/543Lipids, e.g. triglycerides; Polyamines, e.g. spermine or spermidine
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    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/08Peptides having 5 to 11 amino acids
    • A61K38/095Oxytocins; Vasopressins; Related peptides
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    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/164Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from bacteria
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    • A61K38/1703Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
    • A61K38/1709Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
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    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/18Growth factors; Growth regulators
    • A61K38/1825Fibroblast growth factor [FGF]
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    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/18Growth factors; Growth regulators
    • A61K38/1841Transforming growth factor [TGF]
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    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
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    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
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    • A61K47/542Carboxylic acids, e.g. a fatty acid or an amino acid
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/235Saturated compounds containing more than one carboxyl group
    • C07C59/245Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
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    • C07C59/235Saturated compounds containing more than one carboxyl group
    • C07C59/245Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
    • C07C59/285Polyhydroxy dicarboxylic acids having five or more carbon atoms, e.g. saccharic acids
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    • C12N15/00Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
    • C12N15/09Recombinant DNA-technology
    • C12N15/11DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
    • C12N15/113Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing
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    • C12N2310/00Structure or type of the nucleic acid
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    • C12N2310/00Structure or type of the nucleic acid
    • C12N2310/30Chemical structure
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    • C12N2310/351Conjugate

Abstract

Se refiere a un conjugado de GDF15 que comprende una biomolecula enlazada a un acido graso por medio de un enlazador, en donde en acido graso tiene las siguientes formulas A1, A2 o A3; donde R1 es CO2H o H; R2, R3 y R4 son H, OH, entre otros; Ak es alquileno de 6 a 30 atomos de carbono ramificado; n, m y p son enteros entre 6 y 30 o amidas, entre otros. Es un acido preferente: acido 2-undecil-manolico, entre otros. Tambien se refiere a una combinacion y una composicion farmaceutica que la comprende. Dicho conjugado es util en el tratamiento de enfermedades metabolicas, diabetes mellitus tipo 2, pancreatitis, entre otrosIt refers to a GDF15 conjugate that comprises a biomolecule linked to a fatty acid through a linker, wherein in fatty acid it has the following formulas A1, A2 or A3; where R1 is CO2H or H; R2, R3 and R4 are H, OH, among others; Ak is alkylene of 6 to 30 branched carbon atoms; n, m and p are integers between 6 and 30 or amides, among others. It is a preferred acid: 2-undecyl-manolic acid, among others. It also refers to a combination and a pharmaceutical composition comprising it. This conjugate is useful in the treatment of metabolic diseases, type 2 diabetes mellitus, pancreatitis, among others.

PE2016002771A 2014-06-23 2015-06-18 NOVEL FATTY ACIDS AND THEIR USE IN CONJUGATION WITH BIOMOLECULES PE20171095A1 (en)

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Application Number Priority Date Filing Date Title
US201462015862P 2014-06-23 2014-06-23
US201462082327P 2014-11-20 2014-11-20
US201562107016P 2015-01-23 2015-01-23

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PE20171095A1 true PE20171095A1 (en) 2017-08-07

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US (4) US10588980B2 (en)
EP (2) EP3988170A1 (en)
JP (5) JP6636959B2 (en)
KR (2) KR20230056796A (en)
CN (3) CN114133443A (en)
AP (1) AP2016009585A0 (en)
AU (1) AU2015280351C1 (en)
CA (1) CA2953480A1 (en)
CL (1) CL2016003281A1 (en)
CR (1) CR20160596A (en)
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DK (1) DK3157571T3 (en)
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HK (1) HK1232160A1 (en)
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MA (1) MA40278A (en)
MX (1) MX367520B (en)
MY (1) MY193993A (en)
PE (1) PE20171095A1 (en)
PH (1) PH12016502294B1 (en)
PL (1) PL3157571T3 (en)
PT (1) PT3157571T (en)
RS (1) RS62907B1 (en)
SG (2) SG10201912965TA (en)
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